Molecule of the Month
January 2022
The Quest for the Best - A SAR Study of Antiparasitic Ruthenium(II) Compounds

A library of 54 ruthenium derivatives based on the trithiolato-bridged dinuclear ruthenium(II)-arene scaffold [(η6-arene)2Ru2(μ2-SR1)2(μ2-SR2)]+) was synthesized by introducing chemical modifications at the level of bridge thiols.
A three-step screening of the compounds was realized (i) activity against T. gondii and assessment of toxicity in non-infected HFF host cells; (ii) IC50 measurements and (iii) studies on the effects in murine splenocytes.
The compound [(η6-p-MeC6H4Pri)2Ru2(μ2-SC6H4-o-CF3)2(μ2-SC6H4-p-OH)]Cl exhibited the most favorable features.

This work was carried out in the group of Prof. Julien Furrer.

References:

  • E. Paunescu, G. Boubaker, O. Desiatkina, N. Anghel, Y. Amdouni, A. Hemphill, J. Furrer;
    "The quest of the best - A SAR study of trithiolato-bridged dinuclear Ruthenium(II)-Arene compounds presenting antiparasitic properties"
    Eur. J. Med. Chem., 2021, 222, 113610/1-21; doi:10.1016/j.ejmech.2021.113610.